Metocinium iodide, a spasmolytic agent, is an antagonist of muscarinic acetylcholine receptors. The drug is used in patients with irritable bowel syndrome.

Tibalosin is a phenylethylamine derivative patented by Continental Pharma as a potent vasodilator. Tibalosine interacts specifically with alpha- and beta-adrenergic receptors and calcium channel binding sites. In preclinical models, Tibalosin exerts favor influences on arterial pressure in the hypertensive animal. The drug has acceptable toxicity in experimental animals and has been well tolerated by normal human subjects in daily doses of up to 200 mg.

Tisocromide exerts antihypoxic and antidepressant action. The details regarding mechanism of action and use are not available.

Besulpamide has been developed as a diuretic agent.

Treptilamine is a spasmolytic and anticholinergic agent. In the pilot study systolic blood pressure in volunteers decreased significantly 5 to 15 min after intravenous application of the substance for 5 or 30 min. No alteration of circulation was observed after oral application at any dose. All volunteers felt tired. A significant decrease of systolic blood pressure (15 mmHg for 10 min immediately after application) occurred after 15 mg of substance were applied intravenous in the double-blind study. Two of five volunteers recorded a burning sensation in the venous wall which was followed by drowsiness. One volunteer felt increasingly tired after oral application. No influence of the substance could be seen on the clinicochemical parameters examined. The drug treptilamine hydrochloride changes the diameter of the pupils.

Pumitepa is a purine derivative patented by All-Union Scientific-Research Chemical-Pharmaceutical Institute as cancerolytic. Although the exact mechanism of action of pumitepa has yet to be fully elucidated, this agent appears to work through alkylation, thereby causing DNA damage and cell cycle arrest. In in vitro studies, Pumitepa prolonged the mitotic cycle in human embryo fibroblasts by 2.5-3 hr, primarily by prolonging the start of phase G1. Pumitepa induced similar types of chromosomal aberrations in cells of all phases of the mitotic cycle. Chromosomes in phase S were the most sensitive for Pumitepa, followed by chromosomes in phases G1 and G2.

AstraZeneca R&D Charnwood (formerly Astra Charnwood, a subsidiary of AstraZeneca) was developing sibenadet (Viozan, AR-C68397AA) for the potential treatment of chronic obstructive pulmonary disease and asthma. Sibenadet is a dual D2 dopamine receptor, beta2-adrenoceptor agonist that combines bronchodilator activity with the sensory afferent modulating effects associated with D2-receptor agonism. Development of sibenadet has been discontinued due to disappointing efficacy findings.

Tumor hypoxia remains one of the greatest challenges in the treatment of solid tumors, as cancer cells in these regions are resistant to killing by radiation therapy and most anticancer drugs. Tirapazamine (3-Amino-1,2,4-benzotriazine-1,4-dioxide or SR 4233) is a cytotoxic drug with selective toxicity towards hypoxic mammalian cells. Under both aerobic and hypoxic conditions, tirapazamine is reduced by an intracellular reductase to form a highly reactive radical, which can cause DNA single- and double-strand breaks. In addition, tirapazamine under hypoxic conditions reduces the activity of topoisomerase II and stabilizes DNA topoisomerase II cleavable complexes, and these complexes remain bound to DNA. Despite the very promising results obtained in various preclinical studies and early-Phase clinical trials, several Phase III trials have failed to demonstrate any survival benefit of adding tirapazamine to chemotherapy or radiation therapy of cancers.

Tifenazoxide is a thiadiazine derivative patented by Novo Nordisk A/S as the opener of the KATP-regulated potassium channels useful in the treatment of the endocrine system diseases. Tifenazoxide is a selective opener of the beta-cell type (SUR1 / Kir6.2) KATP channel that characterized as competitive inhibitors of glibenclamide binding to membranes of HEK293 cells expressing human SUR1/Kir6.2and as potent inhibitors of insulin release in isolated rat islets. In clinical trials, Tifenazoxide administration leads to a decrease in insulin concentrations 1 h post-dose. This was accompanied by an increase in glucose and growth hormone concentrations (NS), but not of glucagon. During the OGTT a dose-dependent reduction in the 2 h glucose value was observed.